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. 2014 Aug 28;171(18):4255–4272. doi: 10.1111/bph.12782

Table 2.

Summary of ex vivo occupancies in the rat and in vitro binding affinities of vortioxetine

Target Ex vivo occupancy in the rat ED50 (mg·kg−1) [95% CI] In vitro binding affinity, Ki (nM)
Rat Human
5-HT3 0.004 [0.0016–0.011] 1.1 3.7
5-HT7 NC 190 19
5-HT1D ND 3.7 54
5-HT1B 2.3 [1.7–3.2] 16 33
5-HT1A NC 230 15
SERT 0.3 [0.24–0.37] 8.6 1.6

The ex vivo occupancy ED50 values in the rat were derived based on occupancy–dose curves of vortioxetine for the 5-HT3, 5-HT7, 5-HT1B, 5-HT1A receptors and the SERT as shown in Figure 1. The previously published in vitro binding affinities (Bang-Andersen et al., 2011; Mørk et al., 2012) are also shown in order to highlight the species differences for some of the targets. NC, not calculated due to limited range; ND, not determined.